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Iranian Journal of Pharmaceutical Research
Volume 7, Issue 1, December 2008, Pages 29-33
Synthesis and antidepressant activity of N-substituted
imidazole-5-carboxamides in forced swimming test model
Hadizadeh, F.ab, Hosseinzadeh, H.ab , Motamed-Shariaty, V.-S.b, Seifi, M.b, Kazemi, S.b
a Department of Medicinal Chemistry, Pharmacy Faculty, Mashhad University of Medical Sciences, Mashhad, Iran
b Biotechnology and Pharmaceutical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran
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Abstract
Moclobemide is a selective and reversible monoamine oxidase-A inhibitor, which is used as an antidepressant. Three
moclobemide analogues were synthesized by replacing moclobemide phenyl ring with substituted imidazoles. So, N[(4-morpholinyl) ethyl)]-1-benzyl-2-(alkylthio) -1H-imidazole-5-carboxamides (7a-c) were synthesized and studied for
the antidepressant activity using forced swimming test in mice. Analogues 7a-c were found to be more potent than
moclobemide. Minimum effective doses for moclobemide and analogues 7a-c were found to be 20, 2.5, 1.25 and 2.5
mg/kg i.p. respectively. Copyright © 2008 by School of Pharmacy Shaheed Beheshti University of Medical Sciences
and Health Services.
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Author keywords
Antidepressant; Forced swimming model; Imidazolecarboxamides; MAOIs
Indexed Keywords
EMTREE drug terms: antidepressant agent; moclobemide; monoamine oxidase inhibitor; n [(4 morpholinyl)ethyl] 1
benzyl 2 (alkylthio) 1h imidazole 5 carboxamide derivative; n [2 (4 morpholinyl)ethyl] 1 benzyl 2 (benzylthio) 1h
imidazole 5 carboxamide; n [2 (4 morpholinyl)ethyl] 1 benzyl 2 (ethylthio) 1h imidazole 5 carboxamide; n [2 (4
morpholinyl)ethyl] 1 benzyl 2 (methylthio) 1h imidazole 5 carboxamide
EMTREE medical terms: animal experiment; animal model; article; chemical modification; controlled study; drug
activity; drug dose comparison; drug efficacy; drug potency; drug structure; drug synthesis; forced swimming test;
immobilization; LD 50; male; mouse; nonhuman
Chemicals and CAS Registry Numbers: moclobemide, 71320-77-9
ISSN: 17350328Source Type: Journal Original language: English
Document Type: Article